RU2448976C2 - Hcv/hiv inhibitors and their application - Google Patents
Hcv/hiv inhibitors and their application Download PDFInfo
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- RU2448976C2 RU2448976C2 RU2008144299/04A RU2008144299A RU2448976C2 RU 2448976 C2 RU2448976 C2 RU 2448976C2 RU 2008144299/04 A RU2008144299/04 A RU 2008144299/04A RU 2008144299 A RU2008144299 A RU 2008144299A RU 2448976 C2 RU2448976 C2 RU 2448976C2
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Abstract
FIELD: medicine, pharmaceutics.
SUBSTANCE: in claim described are organic compounds of formula I where radicals are given in description, which are applicable for elimination, prevention or alleviation of one or more symptoms, associated with HCV disorders.
EFFECT: obtaining pharmaceutical composition which possesses inhibiting activity with respect to NS3-4 HCV serinprotease, including formula I compound and pharmaceutically acceptable carrier.
30 cl, 25 ex, 2 tbl
Description
Claims (2)
или его фармацевтически приемлемая соль или его стереоизомер;
в которой у равен 1;
n равен 1;
R14 обозначает С(O);
R1 выбран из группы, включающей Н и С1-С4-алкил;
R2 выбран из группы, включающей С1-С4-алкил, С(O)С1-С4-алкил, С(O)ОС1-С4-алкил и С3-С6-циклоалкил-С0-С4-алкил;
или R1 и R2 вместе образуют циклопропановое кольцо, где циклопропановое кольцо может быть дополнительно замещено один или более раз;
W также выбран из группы, включающей С(O)-С(O)Н, C(=N-O-R24)-C(O)-аминогруппу, С(O)-С(O)-аминогруппу, C(O)NR24S(O)pR24, C(O)NR24S(O)pN(R24)2 и С(O)-[С(O)]а-гетероциклил, где гетероциклил может быть один или более раз независимо замещен арилом, C1-C4-алкилом, С1-С4-алкилом, замещенным одним или более атомами галогена, или С3-С6-циклоалкилом, где а равно 0 или 1, где каждый R24 независимо выбран из водорода или из группы, включающей С1-С4-алкил, С3-С6-циклоалкил-С0-С4-алкил, замещенный или незамещенный арил и замещенный или незамещенный гетероциклил, каждый из которых может быть один или более раз независимо замещен атомом галогена или C1-C4-алкилом;
V выбран из группы, включающей -Q1-Q2, где Q1 отсутствует, обозначает С(O), N(H), N(С1-С4-алкил), C=N(CN), C=N(SO2CH3), C=NCOH-C1-C4-алкил или C=N-COH, и Q2 обозначает водород или выбран из группы, включающей С1-С4-алкил, O-С1-С4-алкил, NH2, N(Н)-С1-С4-алкил, N(C1-C4-алкил)2, SО2-арил, SO2-С1-С4-алкил, С3-С6-циклоалкил-С0-С4-алкил, арил, гетероарил и гетероциклил, каждый из которых может быть один или более раз независимо замещен атомом галогена, С1-С4-алкилом, C1-C4-алкилом замещенным одним или более атомами галогена, или С3-С6-циклоалкилом;
р равен 0, 1 или 2;
R3 выбран из группы, включающей водород и С1-С4-алкил;
двухвалентный остаток:
выбран из группы, включающей:
, , ,
,
, , , ,
, ,
, , ,, ,
R8, R9 и R10 каждый независимо выбран из группы, включающей водород, С1-С4-алкил и С3-С6-циклоалкил-С0-С4-алкил;
R11 обозначает Н;
R12 обозначает С3-С6-циклоалкил; и
R13 обозначает Н;
где арил означает 5- и 6-членные моно- или полициклические ароматические группы;
гетероциклил означает 5-10-членный ароматический или неароматический гетероциклил, содержащий от 1 до 4 гетероатомов, выбранных из О, N и S;
и
гетероарил означает моноциклическое или бициклическое кольцо, содержащее до 7 атомов в каждом кольце, в котором по меньшей мере одно кольцо является ароматическим и содержит от 1 до 4 гетероатомов, выбранных из О, N и S.1. The compound of formula I:
or a pharmaceutically acceptable salt thereof or a stereoisomer thereof;
in which y is 1;
n is 1;
R 14 is C (O);
R 1 is selected from the group consisting of H and C 1 -C 4 alkyl;
R 2 is selected from the group consisting of C 1 -C 4 -alkyl, C (O) C 1 -C 4 -alkyl, C (O) OC 1 -C 4 -alkyl and C 3 -C 6 -cycloalkyl-C 0 - C 4 -alkyl;
or R 1 and R 2 together form a cyclopropane ring, where the cyclopropane ring may be further substituted one or more times;
W is also selected from the group consisting of C (O) —C (O) H, C (= NOR 24 ) —C (O) amino group, C (O) —C (O) amino group, C (O) NR 24 S (O) p R 24 , C (O) NR 24 S (O) p N (R 24 ) 2 and C (O) - [C (O)] a- heterocyclyl, where heterocyclyl may be one or more times independently substituted by aryl, C 1 -C 4 alkyl, C 1 -C 4 alkyl substituted with one or more halogen atoms, or C 3 -C 6 cycloalkyl, where a is 0 or 1, where each R 24 is independently selected from hydrogen or from the group consisting of C 1 -C 4 alkyl, C 3 -C 6 cycloalkyl-C 0 -C 4 alkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, each of which can is one or more times independently substituted by a halogen atom or C 1 -C 4 alkyl;
V is selected from the group consisting of -Q 1 -Q 2 , where Q 1 is absent, denotes C (O), N (H), N (C 1 -C 4 alkyl), C = N (CN), C = N (SO 2 CH 3 ), C = NCOH-C 1 -C 4 -alkyl or C = N-COH, and Q 2 is hydrogen or is selected from the group consisting of C 1 -C 4 -alkyl, O-C 1 -C 4- alkyl, NH 2 , N (H) -C 1 -C 4 -alkyl, N (C 1 -C 4 -alkyl) 2 , SO 2 -aryl, SO 2 -C 1 -C 4 -alkyl, C 3 -C 6 -cycloalkyl-C 0 -C 4 -alkyl, aryl, heteroaryl and heterocyclyl, each of which may be independently or independently substituted one or more times by a halogen atom, C 1 -C 4 -alkyl, C 1 -C 4 -alkyl substituted one or more halogen atoms, or C 3 -C 6 cycloalkyl;
p is 0, 1 or 2;
R 3 is selected from the group consisting of hydrogen and C 1 -C 4 alkyl;
divalent residue:
selected from the group including:
, , ,
,
, , , ,
, ,
, , , , ,
R 8 , R 9 and R 10 are each independently selected from the group consisting of hydrogen, C 1 -C 4 alkyl and C 3 -C 6 cycloalkyl-C 0 -C 4 alkyl;
R 11 is H;
R 12 is C 3 -C 6 cycloalkyl; and
R 13 is H;
where aryl means 5- and 6-membered mono- or polycyclic aromatic groups;
heterocyclyl means a 5-10 membered aromatic or non-aromatic heterocyclyl containing from 1 to 4 heteroatoms selected from O, N and S;
and
heteroaryl means a monocyclic or bicyclic ring containing up to 7 atoms in each ring, in which at least one ring is aromatic and contains from 1 to 4 heteroatoms selected from O, N and S.
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